Classifications

• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K33/00—Medicinal preparations containing inorganic active ingredients
  • A61K33/20—Elemental chlorine; Inorganic compounds releasing chlorine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
  • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
  • A61K9/00—Medicinal preparations characterised by special physical form
  • A61K9/0012—Galenical forms characterised by the site of application
  • A61K9/0048—Eye, e.g. artificial tears
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L12/00—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor
  • A61L12/08—Methods or apparatus for disinfecting or sterilising contact lenses; Accessories therefor using chemical substances
  • A61L12/10—Halogens or compounds thereof
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L2/00—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor
  • A61L2/02—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor using physical phenomena
  • A61L2/03—Electric current
  • A61L2/035—Electrolysis
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L2/00—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor
  • A61L2/16—Methods or apparatus for disinfecting or sterilising materials or objects other than foodstuffs or contact lenses; Accessories therefor using chemical substances
  • A61L2/18—Liquid substances or solutions comprising solids or dissolved gases
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F1/00—Treatment of water, waste water, or sewage
  • C02F1/46—Treatment of water, waste water, or sewage by electrochemical methods
  • C02F1/461—Treatment of water, waste water, or sewage by electrochemical methods by electrolysis
  • C02F1/46104—Devices therefor; Their operating or servicing
  • C02F1/4618—Devices therefor; Their operating or servicing for producing "ionised" acidic or basic water
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F1/00—Treatment of water, waste water, or sewage
  • C02F1/46—Treatment of water, waste water, or sewage by electrochemical methods
  • C02F1/461—Treatment of water, waste water, or sewage by electrochemical methods by electrolysis
  • C02F1/467—Treatment of water, waste water, or sewage by electrochemical methods by electrolysis by electrochemical disinfection; by electrooxydation or by electroreduction
  • C02F1/4672—Treatment of water, waste water, or sewage by electrochemical methods by electrolysis by electrochemical disinfection; by electrooxydation or by electroreduction by electrooxydation
  • C02F1/4674—Treatment of water, waste water, or sewage by electrochemical methods by electrolysis by electrochemical disinfection; by electrooxydation or by electroreduction by electrooxydation with halogen or compound of halogens, e.g. chlorine, bromine
• • A—HUMAN NECESSITIES
  • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
  • A61L—METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES
  • A61L2202/00—Aspects relating to methods or apparatus for disinfecting or sterilising materials or objects
  • A61L2202/20—Targets to be treated
  • A61L2202/25—Rooms in buildings, passenger compartments
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F2103/00—Nature of the water, waste water, sewage or sludge to be treated
  • C02F2103/02—Non-contaminated water, e.g. for industrial water supply
  • C02F2103/026—Treating water for medical or cosmetic purposes
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F2209/00—Controlling or monitoring parameters in water treatment
  • C02F2209/04—Oxidation reduction potential [ORP]
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F2209/00—Controlling or monitoring parameters in water treatment
  • C02F2209/29—Chlorine compounds
• • C—CHEMISTRY; METALLURGY
  • C02—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F—TREATMENT OF WATER, WASTE WATER, SEWAGE, OR SLUDGE
  • C02F2303/00—Specific treatment goals
  • C02F2303/04—Disinfection

Definitions

• the invention relates to pharmaceutical compositions containing an active ingredient and a carrier, wherein the carrier consists of an electrochemically activated aqueous saline solution.
• Anolyte or ASECA solution is one with that in the not prepublished EP 10 003 555.9 neutral, electrochemically activated salt solution prepared as described in the ASECA method, which is a highly effective disinfectant.
• This activated solution can be obtained by electrolysis of sodium chloride solutions. It can be used in surface disinfection applications such as countertops, tables, floors, etc., for cold disinfecting operations, in agriculture for the removal of microbial organisms, for washing laundry and in swimming pool applications, and even as a prophylactic against athlete's foot.
• a pharmaceutical composition of the above type which comprises, in addition to an active ingredient, a carrier provided by the active ingredient in a separate, separate phase.
• the carrier consists of an electrochemically activated aqueous saline solution and has a content of free chlorine between 1 and 500 mg / l and a redox potential between 150 and 1350 mV with regard to the greatest possible compatibility and coexistence with the second phase containing the active substance.
• the present invention is based on the object, a pharmaceutical composition of the type mentioned in such a way that without unreasonable impairment of the effectiveness of the active ingredient, a particularly high shelf life and long-term stability of the composition is guaranteed.
• the carrier has a content of free chlorine of more than 500 mg / l, preferably of more than 600 mg / l.
• the invention is based on the consideration that just under the use of the EP 2 178 501 basically known provision of the active ingredient in a phase separate from the carrier in the manner of embedding the active substance in it surrounding carrier material, a targeted increase in shelf life is achievable by the carrier is designed in addition to its carrier properties to a particularly extensive preservative effect. This can be achieved by designing the carrier as a biocide or the like, it being possible to ensure reliable partitioning off of the active ingredient from germs or the like precisely because of the embedding of the active ingredient in the surrounding carrier in the manner of a matrix.
• the carrier should, in departure from the in the EP 2 178 501 intended parameters and designed primarily for a particularly high biocidivity or germ killing effect.
• a content of free chlorine in the carrier of more than 500 mg / l, preferably more than 600 mg / l should be set.
• Particularly favorable is a content of free chlorine of 700 mg / l or more, since just from this limit, the carrier is suitable for meeting the requirements for sterility and thus has a particularly extensive preservative effect.
• the desired germ suppression is particularly reliable reachable, and in particular the usual requirement for a disinfectant, namely the reduction of an initial predetermined germ content by at least a factor of 100 000, is readily possible.
• the stated content of free chlorine can be determined in particular by titration in a conventional manner.
• an electrochemically activated aqueous saline solution suitable for use as a carrier in said pharmaceutical composition can be produced particularly advantageously by electrolysis with a cascade-like connection of anode spaces of a plurality of electrolysis cells, as described, for example, in the non-prepublished document EP 10 003 555.9 ,
• the disclosure of this document, in particular with regard to the production of an electrochemically activated aqueous saline solution with a particularly high content of free chlorine, is expressly incorporated ("incorporation by reference").
• the salinity in the saline solution used as the electrolysis medium is available as a further production parameter in addition to the parameters characteristic for the actual electrolysis process (in particular electrolysis current and voltage).
• this salt content is subject to some marginal conditions (in particular, it should be sufficiently high enough to ensure sufficiently high production rates of chlorine in the anolyte at current current strength of the electrolysis), but can be chosen suitably in the nature of a free parameter apart.
• the salt content can be suitably adjusted in order to set a desired osmolarity in the end product and thus to provide a product (for example, isotonic) adapted in this respect to the intended use.
• the redox potential of the intended as a carrier electrochemically activated salt solution is at pH-neutral solutions advantageously at least between +600 mV and + 1000 mV, preferably at least + 800 mV and / or preferably up to + 900 mV, can be acidic Solutions (ie low pH of for example about 2.5) but also accept significantly higher values. This provides, inter alia, a particularly favorable long-term stability of the substance.
• the electrochemical activated salt solution is preferably an alkali metal hypochlorite solution, e.g. As a lithium, sodium or potassium hypochlorite solution. Most preferably, the solution is a sodium hypochlorite solution.
• the electrochemically activated saline solution advantageously has a pH of from 2 to 8, more preferably about 7.
• a pH of from 2 to 5, e.g. B. 2 to 4, 2 to 3 or 2 to 2.8 be favorable.
• Such an acidic representation of the carrier, especially in combination with the stated free chlorine content, is particularly advantageous when the carrier is used as a biocide against bacterial spores.
• the pH may also be 5 to 8, in particular 5.9 to 7.6 and in particular from 6.7 to 7.4.
• the content of chlorate and / or chlorite is preferably below toxic levels, especially less than 10 mg / l chlorite or less than 20 mg / l chlorate.
• the solution is preferably free of detectable amounts of radicals such as OH radicals or ozone.
• the solution is preferably free of heavy metal ions such as Mo ions.
• any medicament suitable for use in human or veterinary medicine can be provided as the active ingredient.
• a hydrophilic or a lipophilic active ingredient and / or a combination of such active ingredients may be provided.
• the active agent be selected from lipophilic or amphiphilic ingredients, that is, ingredients that have a butanol-water partition coefficient of at least 0.5, preferably at least 1.
• the active ingredient comprises a hydrophilic ingredient such as polysaccharide.
• the active ingredient may be selected from agents for the treatment of glaucoma, e.g.
• Prostaglandins such as latanoprost, beta-blockers such as timolol, agents for lowering elevated intraocular pressure such as dorzolamide, drugs for the treatment of dry eye syndrome (ophthalmic humectants) such as hydroxypropylmethylcellulose (hypromellose), hyaluronic acid and other pharmaceutical agents.
• ophthalmic humectants such as hydroxypropylmethylcellulose (hypromellose), hyaluronic acid and other pharmaceutical agents.
• the pharmaceutical composition of the present invention is stabilized against microbial degradation. So the composition is also suitable for multi-use applications. Due to the properties of the carrier, in particular its high biocidivity, the composition can be designed for multi-use applications even without conventional preservatives.
• the preparation has a stability against microbial degradation of preferably at least 6 months, more preferably at least 12, especially 24 or more, months, even when stored at room temperature.
• the anti-microbial activity of the electrochemically activated salt solution can be determined, for example, by measuring the product cxt from the concentration (c) and the exposure time (t) by a method as described by Schleupen, GWF, 1996.
• the preparation may be used for any type of application, e.g. for local or systemic administration.
• the composition is for ocular, nasal, otic, topical, pulmonary, mucosal, oral or intraperitoneal administration, e.g. For administration by injection.
• Preferred compositions are for ocular administration, e.g. For the treatment of glaucoma or dry eye syndrome.
• the composition preferably forms at least two separate phases wherein the active agent is in a first phase and the electrochemically activated salt solution is in a second phase separate from the first phase.
• the first phase may be a solid particle phase, a liquid hydrophobic phase, or a solid or liquid phase having a barrier to the second phase, wherein the second phase formed by the carrier is preferably an aqueous phase.
• the composition may contain an emulsion, e.g. A microemulsion or a liposomal composition or a microcapsule composition or dispersion.
• the active ingredient can be emulsified or dispersed in the presence of the carrier, for.
• a lipophilic carrier and / or a surfactant in the aqueous carrier are present.
• the active ingredient may be physically separate from the electrochemically activated saline solution.
• microemulsions as described in EP 07 008 347.1 which is incorporated herein by reference ("incorporation by reference”).
• the composition may also contain other additives which are conventional per se, e.g. Buffers, excipients, fillers, diluents, etc.
• the pharmaceutical composition according to the invention can preferably be used in human or veterinary medicine.
• an electrochemically activated salt solution of the above type for the cleaning of contact lenses, e.g. As glass or plastic contact lenses.
• the solution may be present without any active ingredient or contain an active agent, e.g. A polymer as described above.
• biocidal or germicidal activity and thus the antimicrobial activity of the anolyte was tested against examples from all known germ groups, namely against bacteria, bacterial spores, non-enveloped viruses, enveloped viruses and fungi and fungal spores.
• experiments were carried out with Staphylococcus aureus, Enterococcus hirae, Eschericia coli, Proteus mirabilis, Pseudomonas aeruginosa, Canida albicans, Aspergillus niger, Mycobacterium terrae and Mycobacterium avium.
• the electrochemically activated salt solution provided as a carrier thus has a comparatively high and comprehensive, ie broadband and biocidal activity detectable against all germ groups.

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• Health & Medical Sciences (AREA)
• Chemical & Material Sciences (AREA)
• Life Sciences & Earth Sciences (AREA)
• Epidemiology (AREA)
• Animal Behavior & Ethology (AREA)
• General Health & Medical Sciences (AREA)
• Public Health (AREA)
• Veterinary Medicine (AREA)
• General Chemical & Material Sciences (AREA)
• Medicinal Chemistry (AREA)
• Chemical Kinetics & Catalysis (AREA)
• Pharmacology & Pharmacy (AREA)
• Organic Chemistry (AREA)
• Environmental & Geological Engineering (AREA)
• Water Supply & Treatment (AREA)
• Electrochemistry (AREA)
• Engineering & Computer Science (AREA)
• Hydrology & Water Resources (AREA)
• Inorganic Chemistry (AREA)
• Ophthalmology & Optometry (AREA)
• Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
• Medicinal Preparation (AREA)

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Cited By (2)

Citations (6)

• 2010
  • 2010-09-16 EP EP10009703A patent/EP2431056A1/fr not_active Withdrawn
• 2011
  • 2011-09-06 WO PCT/EP2011/004470 patent/WO2012034659A2/fr active Application Filing

Patent Citations (7)

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